The present invention relates to new 7.alpha.-acylthio-1.alpha.,2.alpha.-methylene -3-oxo-17.alpha.-pregn-4-ene-21,17 carbolactones, processes for producing them and pharmaceutical preparations containing them as active ingredients.
In treatments with spironolactone there frequently occur undesirable endocrine side effects that are caused by the antiandrogenic and gestagenic activity of spironolactone. For example, the occurrence of gynecomastia is observed in extended treatment of male patients with spironolactone (Smith, W. G., The Lancet 1962, p 886; Mann, N. M., JAMA 1963, p 778; Clark, E., JAMA 1965, p 157; Greenblatt, D. J., JAMA 1973, p 82) as well as impotence (Greenblatt, D. J., JAMA 1973, p 82) which can be traced to the antiandrogenic side effect of this compound (Steelman, S. L. et al, Steroids 1963, p 449; Schane, H. P., J. of Clinical Endocrinology and Metabolism 1978, p 691).
The side effects on women treated with spironolactone, such as amenorrhea and menstrual irregularities, on the other hand, are ascribed to the gestagenic side effect of spironolactone. Both side effects can be demonstrated in animal experiments as well as in vitro using the conventional receptor binding test with the androgen or gestogen receptor.